Dorsomorphin 2HCl

Dorsomorphin 2HCl

Catalog Number:
L002369968APE
Mfr. No.:
APE-B1372
Price:
$188
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      • Overview
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          Background

          IC50: Dorsomorphin inhibited BMP4-induced phosphorylation of BMP-responsive SMADs in a dose-dependent manner (half maximal inhibitory concentration (IC50) = 0.47 mM).Bone morphogenetic protein (BMP) signals coordinate developmental patterning and have essential physiological roles in mature organisms. The first known small-molecule inhibitor of BMP signaling, dorsomorphin, were identified in a screen for compounds that perturb dorsoventral axis formation in zebrafish. In vitro: Previoius researchers found that dorsomorphin selectively inhibits the BMP type I receptors ALK2/ALK3/ALK6 leading to block BMP-mediated SMAD1/5/8 phosphorylation, osteogenic differentiation as well as target gene transcription. Using dorsomorphin, they examined the role of BMP signaling in iron homeostasis.dorsomorphin inhibited the systemic iron regulator hepcidin BMP-, hemojuvelin- and interleukin 6–stimulated expression, indicating that BMP receptors regulate hepcidin induction by all of these stimuli [1]. In vivo: The systemic challenge with iron rapidly induced SMAD1/5/8 phosphorylation and hepcidin expression in the liver, while dorsomorphin treatment could blocke SMAD1/5/8 phosphorylation, normalize hepcidin expression and increase serum iron levels. These suggest an crucial physiological role for hepatic BMP signaling in iron-hepcidin homeostasis [1]. Clinical trial: Dorsomorphin is still in preclinical development stage and no clinicl trial is ongoing currently.

      • Properties
        • Alternative Name
          6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine;dihydrochloride
          CAS Number
          1219168-18-9
          Molecular Formula
          C24H25N5O·2HCl
          Molecular Weight
          472.41
          Appearance
          A solid
          Purity
          98.12%
          Solubility
          insoluble in EtOH; insoluble in H2O; ≥11.34 mg/mL in 0.9% NS ; ≥39.93 mg/mL in DMSO:H2O=2:1 ; ≥5.91 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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